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Open AccessArticle

LC-MS/MS Determination and Pharmacokinetic Study of Pedunculoside in Rat Plasma after Oral Administration of Pedunculoside and Ilex rotunda Extract

by 1, 2, 2 and 2,*
1
Cardiovascular Medicine, the First Hospital of Jilin University, Changchun 130021, China
2
Emergency Department, the First Hospital of Jilin University, Changchun 130021, China
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Molecules 2015, 20(5), 9084-9098; https://doi.org/10.3390/molecules20059084
Received: 17 March 2015 / Revised: 12 May 2015 / Accepted: 13 May 2015 / Published: 19 May 2015
(This article belongs to the Section Medicinal Chemistry)
Ilex rotunda is widely used to treat many disorders as a traditional Chinese medicine (TCM) containing 4%–5% pedunculoside (PDC). A rapid, selective, and sensitive liquid chromatography-tandem mass spectrometry method (LC-MS/MS) was developed and validated to determine PDC in rat plasma by using 3β,19α-dihydroxyurs-12-en-28-oic acid 28-β-D-glucopyranosyl ester (DEOG) as an internal standard. The analytes were extracted by protein precipitation and eluted on a C18 chromatography column using a mobile phase of methanol–H2O (70:30, v/v) delivered at a flow rate of 0.6 mL/min. Detection was performed using positive ion electrospray ionization in multiple reaction monitoring modes. The assay was linear over the concentration range of 0.60 ng/mL to 200 ng/mL, with a quantification limit of 0.60 ng/mL. Intra-day and inter-day precisions (%RSD) ranged from 2.12 to 9.51 for PDC, whereas the accuracy was within −7.83%~9.40%. The validated method was successfully applied to the pharmacokinetic study of PDC in rat plasma after oral administration of pure PDC and Ilex rotunda extract (IRE). Pharmacokinetic parameters of PDC in IRE, such as Cmax, AUC0–t, AUC0–∞, t1/2z, and CLz/F, statistically differed from those of the pure monomer (p < 0.01). However, Tmax and MRT showed no significant differences between the two groups. Results suggested that other coexisting components in IRE may decrease the absorption of PDC. Compound-compound interactions between PDC and other herbal extract components can alter the pharmacokinetic behavior of PDC. The study will be helpful in providing references for understanding the action mechanism and clinical application of Ilex rotunda. View Full-Text
Keywords: LC-MS/MS; pedunculoside; pharmacokinetics; Ilex rotunda LC-MS/MS; pedunculoside; pharmacokinetics; Ilex rotunda
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Zhao, W.; Pang, L.; Xu, D.; Zhang, N. LC-MS/MS Determination and Pharmacokinetic Study of Pedunculoside in Rat Plasma after Oral Administration of Pedunculoside and Ilex rotunda Extract. Molecules 2015, 20, 9084-9098.

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